Recent Advances in the Search for Novel 5‐Lipoxygenase Inhibitors

5‐Lipoxygenase (5‐LO) is an important enzyme of the arachidonic acid cascade and catalyses with the help of FLAP, the 5‐LO‐activating protein, the formation of bioactive leukotrienes (LTs). LTs are inflammatory mediators playing a pathophysiological role in different diseases such as asthma, allergic rhinitis as well as cardiovascular diseases and certain types of cancer. Up to now, only one 5‐LO inhibitor is on the market, zileuton for the treatment of asthma. With the rising number of indications for anti‐LT therapy, 5‐LO inhibitor drug development becomes more and more important. This MiniReview gives an update on 5‐LO inhibitors currently under clinical development. Furthermore, the recent advances in the search for novel 5‐lipoxygenase inhibitors with a focus on computational methods are summarized. Currently, licofelone is the compound with the highest clinical development status (completed phase III trials). 5‐LO inhibitor screening programmes based on computational methods could deliver several promising drug‐like new molecules. These activities can be expected to be driven by the newly resolved structure of human 5‐LO in the future, enabling structure‐based drug design. For the prospective drugs in late‐stage clinical development, the future will show their clinical safety and efficacy in the particular diseases.